Fan Ruolan, He Weishen, Fan Yong, Xu Wen, Xu Wei, Yan Guohong, Xu Shaohua
College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, Fujian 350122, PR China.
Biology Department, Boston College, Brighton, MA 02135, USA.
Steroids. 2022 Apr;180:108991. doi: 10.1016/j.steroids.2022.108991. Epub 2022 Feb 23.
Extracting organic compounds from plants and developing derivatives are essential methods for drug discovery. Diosgenin, extracted from Dioscoreaceae plants, is a type of spirostan steroid with various biological effects, including anti-inflammation, neuro-protection, and apoptosis-induction. Many researchers committed their work to the chemical semi-synthesis of diosgenin derivatives to improve diosgenin's therapeutic bioavailability and expand its range of applications in disease treatment and prevention. Biotransformation, a mild whole-cell biocatalysis method, also made crucial contributions to the structural diversity of diosgenin analogs in recent years. Although the structural modification of diosgenin has made significant progress, it lacks a comprehensive review. Here, we review the chemical modification and biotransformation of diosgenin along with the biological evaluation of diosgenin derivatives to provide a reference for the structural modification strategy and pharmaceutical application of diosgenin derivatives.
从植物中提取有机化合物并开发其衍生物是药物发现的重要方法。从薯蓣科植物中提取的薯蓣皂苷元是一种螺甾烷甾体，具有多种生物学效应，包括抗炎、神经保护和诱导细胞凋亡。许多研究人员致力于薯蓣皂苷元衍生物的化学半合成，以提高薯蓣皂苷元的治疗生物利用度，并扩大其在疾病治疗和预防中的应用范围。生物转化作为一种温和的全细胞生物催化方法，近年来也为薯蓣皂苷元类似物的结构多样性做出了重要贡献。尽管薯蓣皂苷元的结构修饰取得了显著进展，但缺乏全面的综述。在此，我们综述了薯蓣皂苷元的化学修饰和生物转化以及薯蓣皂苷元衍生物的生物学评价，为薯蓣皂苷元衍生物的结构修饰策略和药物应用提供参考。
